Table 1.
Review of the pharmacokinetics of lapatinib at the dose of 1250 mg/day, approved by the Food and Drug Administration
Absorption | Oral, not available in IV form |
Tmax | 3–4 hours |
Steady-state Cmax | 2.43 μg/mL |
AUC | 36.2 μg h/mL |
Distribution | Highly bound (>99%) to albumin |
Volume of distribution | > 2200 L |
Metabolism | |
Primary | CYP3A4 (70% of metabolism) |
Secondary | CYP3A5, CYP2C19, CYP2C8 |
Elimination | Primarily hepatic |
Single dose t1/2 | 14.2 hours |
Multiple doses t1/2 | 24 hours |
Abbreviations: t1/2, elimination half-life; AUC, area under the concentration-time curve; IV, intravenous; Tmax, time to peak concentration; Cmax, maximum concentration.